Table 5. Inhibitory effects and IC50 of series II peptide-like ligand binding rhNRP-1 (chemiluminescence detection).
Compound | AA2–AA3 fragment | Inhibition of NRP-1/VEGF-A165 binding [%] |
IC50 [μM] | ||||||
100 μM | 50 μM | 25 μM | 10 μM | 5 μM | 2.5 μM | 1 μM | |||
3 | Dab–Pro | 79.8 ± 0.8 | 76.6 ± 0.9 | 70.4 ± 0.5 | 58.6 ± 1.4 | 43.7 ± 0.7 | 31.4 ± 0.5 | 13.8 ± 0.3 | 8.9 ± 0.8 (ref. 40) |
11 | Dab–Hyp | 78.6 ± 0.7 | 76.0 ± 0.6 | 67.3 ± 1.5 | 54.3 ± 2.0 | 36.0 ± 0.0 | 22.3 ± 1.5 | 22.5 ± 0.3 | 9.2 ± 0.7 a |
12 | Dab–Aze | 78.8 ± 0.6 | 75.8 ± 0.3 | 69.1 ± 0.3 | 49.6 ± 4.2 | 30.1 ± 1.8 | 12.9 ± 1.4 | 7.7 ± 1.0 | 11.7 ± 1.2 b |
13 | Dab–ΔPro | 87.1 ± 0.6 | 84.4 ± 0.3 | 78.1 ± 1.0 | 70.7 ± 0.3 | 58.0 ± 0.8 | 44.8 ± 0.4 | 29.9 ± 1.5 | 4.3 ± 0.2 c |
14 | Dab–Oic | 83.0 ± 0.3 | 79.5 ± 0.5 | 77.7 ± 1.3 | 63.4 ± 1.9 | 52.3 ± 3.3 | 50.9 ± 3.2 | 37.7 ± 2.1 | 2.3 ± 0.2 d |
15 | Dab–Piz | 51.8 ± 0.4 | 46.0 ± 0.6 | 34.8 ± 0.3 | 20.8 ± 0.6 | — | — | — | 80.5 ± 2.0 e |
16 | Dab–Tic | 0.0 ± 3.2 | 17.2 ± 1.4 | 35.0 ± 1.2 | 31.5 ± 2.5 | — | — | — | ≫100 |
alog IC50 = –5.03 ± 0.07.
blog IC50 = –4.97 ± 0.05.
clog IC50 = –5.54 ± 0.04.
dlog IC50 = –5.65 ± 0.08.
elog IC50 = –4.09 ± 0.07. R2 was between 0.92–0.98. Results are presented as the mean ± SEM.